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irinotecan : ウィキペディア英語版
irinotecan

Irinotecan (Camptosar, Pfizer; Campto) is a drug used for the treatment of cancer.
Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1. In chemical terms, it is a semisynthetic analogue of the natural alkaloid camptothecin.
Its main use is in colon cancer, in particular, in combination with other chemotherapy agents. This includes the regimen FOLFIRI, which consists of infusional 5-fluorouracil, leucovorin, and irinotecan.
Irinotecan received accelerated approval by the U.S. Food and Drug Administration (FDA) in 1996〔New York Times Article http://www.nytimes.com/1996/06/18/science/new-cancer-drug-approved.html〕 and full approval in 1998.〔FDA Review Letter http://www.accessdata.fda.gov/drugsatfda_docs/appletter/1998/20571s8ltr.pdf〕 During development, it was known as CPT-11.
==Mechanism==

Irinotecan is activated by hydrolysis to SN-38, an inhibitor of topoisomerase I. This is then inactivated by glucuronidation by uridine diphosphate glucoronosyltransferase 1A1 (UGT1A1). The inhibition of topoisomerase I by the active metabolite SN-38 eventually leads to inhibition of both DNA replication and transcription.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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